Facile synthesis of new carbon-11 labeled conformationally restricted rivastigmine analogues as potential PET agents for imaging AChE and BChE enzymes

被引：6
作者：
Wang, Min [1 ]
Wang, Ji-Quan [1 ]
Gao, Mingzhang [1 ]
Zheng, Qi-Huang [1 ]
机构：
[1] Indiana Univ, Sch Med, Dept Radiol, Indianapolis, IN 46202 USA
来源：
APPLIED RADIATION AND ISOTOPES | 2008年 / 66卷 / 04期
关键词：
acetylcholinesterase (AChE); butyrylcholinesterase (BChE); positron emission tomography (PET); rivastigmine; conformationally restricted analogues; carbon-11; imaging;
D O I：
10.1016/j.apradiso.2007.11.005
中图分类号：
O61 [无机化学];
学科分类号：
070301 ; 081704 ;
摘要：
Rivastigmine is a newer-generation inhibitor with a dual inhibitory action on both acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes, and is used for the treatment of AChE- and BChE-related diseases such as brain Alzheimer's disease and cardiovascular disease. New carbon-11 labeled conformationally restricted rivastigmine analogues radiolabeled quaternary ammonium triflate salts, (3aR,9bS)-1-[C-11]methyl-1-methyl-6-(methylcarbarnoyloxy)-2,3,3a,4,5,9b-hexahydro-1H-benzo[g]indolium triflate ([C-11]8) and (3aR,9bS)-1-[C-11]methyl-1-methyl-6-(heptylcarbamoyloxy)-2,3,3a,4,5,9b-hexahydro-1H-benzo[g]indolium triflate ([C-11]9), were designed and synthesized as potential positron emission tomography (PET) agents for imaging AChE and BChE enzymes. The appropriate precursors were labeled with [C-11]CH3OTf through N-[C-11]lmethylation, and the target tracers were isolated by solid-phase extraction (SPE) using a cation-exchange CM Sep-Pak cartridge in 40-50% radiochemical yields decay corrected to end of bombardment (EOB), 15-20min overall synthesis time, and 148-222GBq/mu mol specific activity at EOB. (c) 2007 Elsevier Ltd. All rights reserved.
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收藏
页码：506 / 512
页数：7
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